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Hsp90 抑制剂在选择性抗疟药物设计中的应用:过去、现在和未来。

Inhibitors of the Hsp90 towards Selective Antimalarial Drug Design: The Past, Present and Future.

机构信息

Department of Biochemistry, Stellenbosch University, Stellenbosch 7600, South Africa.

出版信息

Cells. 2021 Oct 22;10(11):2849. doi: 10.3390/cells10112849.

Abstract

Malaria is still one of the major killer parasitic diseases in tropical settings, posing a public health threat. The development of antimalarial drug resistance is reversing the gains made in attempts to control the disease. The parasite leads a complex life cycle that has adapted to outwit almost all known antimalarial drugs to date, including the first line of treatment, artesunate. There is a high unmet need to develop new strategies and identify novel therapeutics to reverse antimalarial drug resistance development. Among the strategies, here we focus and discuss the merits of the development of antimalarials targeting the Heat shock protein 90 (Hsp90) due to the central role it plays in protein quality control.

摘要

疟疾仍然是热带地区主要的致死性寄生虫病之一,对公共卫生构成威胁。抗疟药物耐药性的发展正在逆转为控制这种疾病所取得的成果。寄生虫的生命周期非常复杂,它已经适应了几乎所有已知的抗疟药物,包括一线治疗药物青蒿琥酯。因此,迫切需要开发新的策略和识别新的疗法来逆转抗疟药物耐药性的发展。在这些策略中,我们重点讨论了针对热休克蛋白 90(Hsp90)开发抗疟药物的优点,因为它在蛋白质质量控制中起着核心作用。

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